US5902806AExpiredUtility

Crystalline vitamin D derivative

82
Assignee: SUMITOMO PHARMAPriority: Feb 28, 1996Filed: Feb 24, 1997Granted: May 11, 1999
Est. expiryFeb 28, 2016(expired)· nominal 20-yr term from priority
C07C 401/00
82
PatentIndex Score
29
Cited by
25
References
12
Claims

Abstract

A crystalline (5Z,7E,23S)-26,26,26,27,27,27-hexafluoro-9,10-secocholesta-5,7,10(19)-trien-1 alpha ,3 beta ,23,25-tetraol monohydrate has an excellent preservation stability, and is therefore useful as a medicine for treating or preventing bone diseases, tumor or psoriasis.

Claims

exact text as granted — not AI-modified
What we claim is: 
     
       1. A crystalline vitamin D derivative of formula (1): ##STR4## 
     
     
       2. A crystalline vitamin D derivative according to claim 1, which shows a powder X-ray diffraction spectrum in average values of interplanar spacing d and relative intensity as given in the following table:   ______________________________________
Inter-                 Inter-
planar    Relative     planar   Relative
spacing d intensity    spacing d
                                intensity
______________________________________
15.77     100          3.92     7
10.80     10           3.77     10
9.58      6            3.73     8
8.37      15           3.67     5
7.89      13           3.60     7
7.46      8            3.55     6
6.65      51           3.46     8
6.34      31           3.31     15
5.96      23           3.18     8
5.79      29           2.96     7
5.34      54           2.92     6
4.88      18           2.76     5
4.78      25           2.70     5
4.54      29           2.66     6
4.32      13           2.63     7
4.23      18           2.54     5
4.17      13           2.48     5
______________________________________
     
     
     
       3. A method for preparing a crystalline vitamin D derivative according to claim 1, which comprises the step of: subjecting a non-crystalline vitamin D derivative of formula (2): ##STR5## to crystallization treatment in an organic solvent having water added thereto. 
     
     
       4. A medicament for the treatment of a disease due to abnormality in calcium absorption, transportation or metabolism, tumor or psoriasis, which comprises an effective amount of a crystalline vitamin D derivative according to claim 1 as an active ingredient. 
     
     
       5. A medicament for the treatment of psoriasis, which comprises an effective amount of a crystalline vitamin D derivative according to claim 1 as an active ingredient. 
     
     
       6. A pharmaceutical composition comprising a crystalline vitamin D derivative according to claim 1 as an active ingredient and a pharmaceutically acceptable material. 
     
     
       7. A pharmaceutical composition according to claim 6, which is in the form of an external formulation. 
     
     
       8. A pharmaceutical composition according to claim 6, which contains an ultraviolet light absorption agent. 
     
     
       9. A pharmaceutical composition according to claim 8, wherein said ultraviolet light absorption agent is selected from benzophenones, 4-aminobenzoic acids, cinnamic acids, salicylic acids, anthranylic acids, vitamin Es, 1-(4-methoxyphenyl)-3-(4-t-butylphenyl)propan-1,3-dione, urocanic acids, and camphor. 
     
     
       10. A method for preparing a pharmaceutical composition which comprises the step of mixing a crystalline vitamin D derivative according to claim 1 with a pharmaceutically acceptable material. 
     
     
       11. A method of treating a disease caused by an abnormality in calcium absorption, transportation or metabolism, tumor or psoriasis, comprising administering to a person in need thereof, a pharmaceutical composition according to claim 6. 
     
     
       12. A method of treating psoriasis, comprising administering to a person in need thereof, a pharmaceutical composition according to claim 6.

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